125174-30-3

Upstream product

• 619-08-9 2-chloro-4-nitrophenol 
• 106-93-4 ethylene dibromide 

Downstream Products

• 125174-45-0 [2-(2-Chloro-4-nitro-phenoxy)-ethyl]-methyl-[2-(4-nitro-phenyl)-ethyl]-amine 
• 177597-12-5 1-(2-chloro-4-nitrophenoxy)-2-[N-(3,4-dimethoxyphenethyl)-N-methylamino]ethane 
• 177597-13-6 1-(4-amino-2-chlorophenoxy)-2-[N-(3,4-dimethoxyphenethyl)-N-methylamino]ethane 
• 125174-63-2 4-(2-{[2-(4-Amino-phenyl)-ethyl]-methyl-amino}-ethoxy)-3-chloro-phenylamine 
• 115256-43-4 N-[3-Chloro-4-(2-{[2-(4-methanesulfonylamino-phenyl)-ethyl]-methyl-amino}-ethoxy)-phenyl]-methanesulfonamide 
• 1408285-00-6 3-chloro-4-[2-(2-oxa-6-aza-spiro[3.3]hept-6-yl)-ethoxy]-phenylamine 
• 1408284-60-5 3-{3-chloro-4-[2-(2-oxa-6-aza-spiro[3.3]hept-6-yl)-ethoxy]-phenyl}-6-(4-chloro-phenyl)-3H-thieno[3,2-d]pyrimidin-4-one 
• 1408285-01-7 6-[2-(2-chloro-4-nitro-phenoxy)-ethyl]-2-oxa-6-aza-spiro[3.3]heptane 

Relevant academic research and scientific papers

Design, synthesis, and biological study of 4-[(2-nitroimidazole-1h-alkyloxyl)aniline]-quinazolines as EGFR inhibitors exerting cytotoxicities both under normoxia and hypoxia

Purpose: In order to get novel EGFR inhibitors exerting more potency in tumor hypoxia than in normoxia. Methods: A series of 4-[(2-nitroimidazole-1H-alkyloxyl)aniline]-quinazolines were designed and synthesized, and their in vitro cytotoxicity and EGFR inhibitory activity were evaluated. Molecule docking study was performed for the representative compound. Results: The structure-activity relationship (SAR) studies revealed that compounds bearing both meta-chloride and para-(2-nitroimidazole-1H-alkyloxy) groups on the aniline displayed potent inhibitory activities both in enzymatic and cellular levels. The most promising compound 16i potently inhibited EGFR with an IC50 value of 0.12 μM. Meanwhile, it manifested more potent cytotoxicity than the positive control lapatinib under tumor normoxia and hypoxia conditions (IC50 values of 1.59 and 1.09 μM against A549 cells, 2.46 and 1.35 μM against HT-29 cells, respectively). The proposed binding model of 16i in complex with EGFR was displayed by the docking results. Conclusion: This study provides insights for developing hypoxia-activated kinase inhibitors.

OXETANE SUBSTITUTED THIENO PYRIMIDINONES

The present invention provides a compound of Formula (I) or pharmaceutically acceptable salt thereof wherein is selected from the group consisting of unsubstituted aryl and heteroaryl groups and aryl and heteroaryl groups substituted with Q; Q represents

BETA-KETOAMIDE COMPOUNDS HAVING AN MCH-ANTAGONISTIC EFFECT AND MEDICAMENTS CONTAINING SAID COMPOUNDS

The invention relates to β-ketoamide compounds of general formula (I) wherein the groups and radicals A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the designations cited in patent claim 1. The invention also relates to medicaments containing at least one inventive amide. As a result of the MCH receptor antagonistic activity, the inventive medicaments are suitable for treating metabolic disorders and/or eating disorders, especially adipositas, bulimia, anorexia, hyperphagia and diabetes.

Beta-ketoamide compounds with MCH antagonistic activity

Compounds of formula I wherein the groups and residues A, B, b, X, Y, Z, R1, R2, R3, R5a and R5b have the meanings given in claim 1. The invention further relates to pharmaceutical compositions containing at least one amide according to the invention. As a result of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia, and diabetes.

Amine derivatives, processes for producing them and a use of them as antiarrhythmic drugs

PCT No. PCT/JP95/01138 Sec. 371 Date May 27, 1997 Sec. 102(e) Date May 27, 1997 PCT Filed Jun. 7, 1995 PCT Pub. No. WO96/04231 PCT Pub. Date Feb. 15, 1996Novel amine derivatives of the following general formula (I): (wherein) A may denote -(CH2)-O-, -(CH2)2-O-, or -(CH2)2-NH-; B may denote -(CH2)2-; R1 may denote a hydrogen atom, a halogen atom, a nitro group, a 1-pyrrolyl group, an acetamido group, an amino group or a dimethylamino group; R2 may denote a hydrogen atom or a nitro group; R3 and R4 may denote a hydrogen atom; R8a and R8b which are the same may denote a chlorine atom or a methoxy group; R9 may denote a hydrogen atom or an amino group; R may denote a methyl group; and X may denote a methanesulfonamido group, a 1-imidazolyl group or a nitro group or a salts thereof are useful as antiarrhythmic drugs.

Synthesis and biological activity of KCB-328 and its analogues: Novel class III antiarrhythmic agents with little reverse frequency dependence

A series of 3,4-dimethoxyphenethylamine derivatives was prepared, and their prolongation effects on effective refractory period of contractile response (ERPc) and action potential duration (APD) in isolated guinea-pig papillary muscles at 1 Hz and 3 Hz were examined. SAR studies led to the identification of KCB-328 (51) which is a novel class III antiarrhythmic agent with little reverse frequency dependence.